【药物名称】Rasagiline mesilate, TVP-1012, (+)-AGN-1135, Agilect
化学结构式(Chemical Structure):
参考文献No.15419
标题:R-Enantiomers of N-propargyl-1-aminoindan cpds., their preparation and pharmaceutical compsns. containing them
作者:Youdim, M.B.H.; Finberg, J.P.M.; Levy, R.; Sterling, J.; Lerner, D.; Berger-Paskin, T. (Teva Pharmaceutical Industries Ltd.)
来源:EP 0436492; JP 1991294248; US 5453446
合成路线图解说明:

Rasagiline can be obtained by two related ways: 1) The alkylation of racemic 1-aminoindane with propagyl chloride (II) and K2CO3 in hot acetonitrile gives the racemic secondary amine (III), which is submitted to optical resolution by chromatography over Chiracel OJ and eluting with hexane/isopropanol (90:10). 2) By alkylation of (R)-1-aminoindane (IV) with propargyl chloride (or bromide) (II) as before.

参考文献No.26910
标题:R-Enantiomer of N-propargyl-1-aminoindan, salts, compsns. and uses thereof
作者:Youdim, M.B.H.; Finberg, J.P.M.; Levy, R.; Sterling, J.; Lerner, D.; Berger-Paskin, T.; Yellin, H.; Veinberg, A. (Teva Pharmaceutical Industries Ltd.)
来源:WO 9511016
合成路线图解说明:

Rasagiline can be obtained by two related ways: 1) The alkylation of racemic 1-aminoindane with propagyl chloride (II) and K2CO3 in hot acetonitrile gives the racemic secondary amine (III), which is submitted to optical resolution by chromatography over Chiracel OJ and eluting with hexane/isopropanol (90:10). 2) By alkylation of (R)-1-aminoindane (IV) with propargyl chloride (or bromide) (II) as before.

参考文献No.371062
标题:Rasagiline
作者:Graul, A.; Casta馿r, J.
来源:Drugs Fut 1996,21(9),903
合成路线图解说明:

Rasagiline can be obtained by two related ways: 1) The alkylation of racemic 1-aminoindane with propagyl chloride (II) and K2CO3 in hot acetonitrile gives the racemic secondary amine (III), which is submitted to optical resolution by chromatography over Chiracel OJ and eluting with hexane/isopropanol (90:10). 2) By alkylation of (R)-1-aminoindane (IV) with propargyl chloride (or bromide) (II) as before.

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